Summary： The underlying mechanism of deguelin regulating the cell cycle in human Burkitt＇s lym phoma cell line Raji cells in vitro, and the cytotoxicity of deguelin to Raji cells and human peripheral blood monocular...Summary： The underlying mechanism of deguelin regulating the cell cycle in human Burkitt＇s lym phoma cell line Raji cells in vitro, and the cytotoxicity of deguelin to Raji cells and human peripheral blood monocular cells （PBMCs） were investigated. The effects of deguelin on the growth of Raji cells were studied by 3-（4, 5-dimethyl-2-thiazolyl）-2,5-diphenyl-2H-tetrazolium （MTT） assay. Apoptosis was detected through Hoechst 33258 staining. The effect of deguelin on the cell cycle of Raji cells was studied by a propidium iodide method. The expression levels of cyclin D1, P21 and pRb were examined by using Western blotting. The results showed that the proliferation of Raji cells was inhibited in the de guelin-treated group, with a 24-h IC5o value of 21.61 nmol/L and a 36-h IC50 value of 17.07 nmol/L. Proliferation in Raji cells was inhibited significantly by deguelin, while little change was observed in PBMCs. Deguelin induced G2/M arrest in Raji cells. The expression of cyclin D1, P21 and pRb was dramatically down-regulated by deguelin in a dose-dependent manner. It was concluded that deguelin could inhibit the proliferation of Raji cells by arresting the cells at GE/M phase and inducing the cell apoptosis. Moreover, deguelin selectively induced apoptosis of Raji cells with low toxicity to PBMCs. The antitumor effects of deguelin were related to the down-regulated expression of cyclin D1, P21 and pRb proteins.展开更多
In order to investigate the anti-cancer effects of deguelin and on K562 and K562/ADM cells in vitro and the underlying molecular mechanism and compare the cytotoxicity of deguelin on K562, K562/ADM cells and human per...In order to investigate the anti-cancer effects of deguelin and on K562 and K562/ADM cells in vitro and the underlying molecular mechanism and compare the cytotoxicity of deguelin on K562, K562/ADM cells and human peripheral blood mononuclear cells （PBMCs）. The effects of deguelin on cell proliferation were assessed by MTT assay. Apoptosis were detected by Annexin V/PI double-labeled cytometry. The effects of deguelin on the cell cycle were studied by a propidium iodide method. Our study showed that deguelin inhibited the proliferation of K562 cell and K562/ADM cell in a time- and dose-dependent manner and had minimal effects on normal human peripheral blood mononuclear cells. The ratio of IC50 value of deguelin of 24 h on K562/ADM cells to K562 cells was only 1.27, which was significantly lower than the ratio of IC50 value of ADM （higher than 20）. Deguelin could induce apoptosis of K562 cells and K562/ADM cells. K562 cells were arrested at G2/M phase while K562/ADM cells were arrested at G0/G~ phase. Our results suggested that deguelin was a novel anti-leukemia agents with high efficacy and low toxicity and it is also a promising agent for reversing drug resistance.展开更多
This article deals with extraction and purification of deguelin,which is a main rotenoid occurred in the root of Derris trifoliate Lour.Deguelin has gained much attention of scientists because of its potential ability...This article deals with extraction and purification of deguelin,which is a main rotenoid occurred in the root of Derris trifoliate Lour.Deguelin has gained much attention of scientists because of its potential ability to inhibit cancer cell proliferation.The dried root powder was extracted with ethanol by ultrasonic-assisted extraction for 30 min,and then filtrated and concentrated to give pasty concentrate.The concentrate was loaded onto silica gel column chromatography subsequently;and the chemical was eluted using a binary solvent mixture of petroleum ether(60-90ºC)-ethyl acetate(4:1,v/v).All tentative identification was carried out by high performance liquid chromatography(HPLC).Most crystal of deguelin was obtained after the fractions mainly containing deguelin were pooled and placed in the dark at 4ºC for three days.With recrystallization from carbon tetrachloride for three times,the purity of deguelin crystal was 99.15%and the yield was 0.55%of the dried weight of D.trifoliate Lour root.展开更多
鱼藤素是大量存在于豆科植物中的一种鱼藤酮类化合物,具有多种生物学活性,如杀虫、抗肿瘤、抗炎、抗病毒、抗糖尿病神经病变以及抗骨质疏松等。然而,高剂量的鱼藤素可导致呼吸抑制、心脏毒性和神经传导阻断等剂量相关的不良影响,这推动...鱼藤素是大量存在于豆科植物中的一种鱼藤酮类化合物,具有多种生物学活性,如杀虫、抗肿瘤、抗炎、抗病毒、抗糖尿病神经病变以及抗骨质疏松等。然而,高剂量的鱼藤素可导致呼吸抑制、心脏毒性和神经传导阻断等剂量相关的不良影响,这推动了负载鱼藤素的新制剂和鱼藤素结构修饰类似物的不断发展。本文通过检索SciFinder、Web of science、PubMed、CNKI等数据库中已发表的关于鱼藤素及其衍生物的相关文献资料,对鱼藤素的来源、生物活性、毒性、及其衍生物的研究进展,特别是针对其抗肿瘤活性的结构修饰与优化研究进行了综述,经分析和归纳总结发现针对鱼藤素的结构修饰主要集中于B、C、E环骨架和A环上的取代基,其目的主要是提高抗肿瘤活性并降低毒性,所得衍生物多数是作为Hsp90 C端抑制剂而表现出优良的抗肿瘤活性。本综述研究将为后续基于鱼藤素的生物活性研究和新药研发,特别是关于鱼藤素及其衍生物在抗肿瘤领域的深入研究和探索提供一定的借鉴和参考。展开更多
Under the guide of living thing active trace,active ingredients having poisonous effect on frematodes grandis and pieris rapae were extracted from amorpha fruitcosa leaves with CH3CH2OH.Five pure compounds were separa...Under the guide of living thing active trace,active ingredients having poisonous effect on frematodes grandis and pieris rapae were extracted from amorpha fruitcosa leaves with CH3CH2OH.Five pure compounds were separated and obtained through purification by column and thin-layer chromatography:6α,12α-Dehgdro-deguelin,6α,12α-Dehgdro-α-toxicarol,（±）-Tephrosin,（-）6-Hgdroxg-6α,12α-Dehydrol-toxicarol and Rotenone.展开更多
基金supported by grants from the National Natural Science Foundation of China(No.30900597)the Science Foundation of Hubei Health Department(No.JX6B08)
文摘Summary： The underlying mechanism of deguelin regulating the cell cycle in human Burkitt＇s lym phoma cell line Raji cells in vitro, and the cytotoxicity of deguelin to Raji cells and human peripheral blood monocular cells （PBMCs） were investigated. The effects of deguelin on the growth of Raji cells were studied by 3-（4, 5-dimethyl-2-thiazolyl）-2,5-diphenyl-2H-tetrazolium （MTT） assay. Apoptosis was detected through Hoechst 33258 staining. The effect of deguelin on the cell cycle of Raji cells was studied by a propidium iodide method. The expression levels of cyclin D1, P21 and pRb were examined by using Western blotting. The results showed that the proliferation of Raji cells was inhibited in the de guelin-treated group, with a 24-h IC5o value of 21.61 nmol/L and a 36-h IC50 value of 17.07 nmol/L. Proliferation in Raji cells was inhibited significantly by deguelin, while little change was observed in PBMCs. Deguelin induced G2/M arrest in Raji cells. The expression of cyclin D1, P21 and pRb was dramatically down-regulated by deguelin in a dose-dependent manner. It was concluded that deguelin could inhibit the proliferation of Raji cells by arresting the cells at GE/M phase and inducing the cell apoptosis. Moreover, deguelin selectively induced apoptosis of Raji cells with low toxicity to PBMCs. The antitumor effects of deguelin were related to the down-regulated expression of cyclin D1, P21 and pRb proteins.
基金This project was supported by a grant from the National Natural Sciences Foundation of China (No. 30472267)
文摘In order to investigate the anti-cancer effects of deguelin and on K562 and K562/ADM cells in vitro and the underlying molecular mechanism and compare the cytotoxicity of deguelin on K562, K562/ADM cells and human peripheral blood mononuclear cells （PBMCs）. The effects of deguelin on cell proliferation were assessed by MTT assay. Apoptosis were detected by Annexin V/PI double-labeled cytometry. The effects of deguelin on the cell cycle were studied by a propidium iodide method. Our study showed that deguelin inhibited the proliferation of K562 cell and K562/ADM cell in a time- and dose-dependent manner and had minimal effects on normal human peripheral blood mononuclear cells. The ratio of IC50 value of deguelin of 24 h on K562/ADM cells to K562 cells was only 1.27, which was significantly lower than the ratio of IC50 value of ADM （higher than 20）. Deguelin could induce apoptosis of K562 cells and K562/ADM cells. K562 cells were arrested at G2/M phase while K562/ADM cells were arrested at G0/G~ phase. Our results suggested that deguelin was a novel anti-leukemia agents with high efficacy and low toxicity and it is also a promising agent for reversing drug resistance.
文摘This article deals with extraction and purification of deguelin,which is a main rotenoid occurred in the root of Derris trifoliate Lour.Deguelin has gained much attention of scientists because of its potential ability to inhibit cancer cell proliferation.The dried root powder was extracted with ethanol by ultrasonic-assisted extraction for 30 min,and then filtrated and concentrated to give pasty concentrate.The concentrate was loaded onto silica gel column chromatography subsequently;and the chemical was eluted using a binary solvent mixture of petroleum ether(60-90ºC)-ethyl acetate(4:1,v/v).All tentative identification was carried out by high performance liquid chromatography(HPLC).Most crystal of deguelin was obtained after the fractions mainly containing deguelin were pooled and placed in the dark at 4ºC for three days.With recrystallization from carbon tetrachloride for three times,the purity of deguelin crystal was 99.15%and the yield was 0.55%of the dried weight of D.trifoliate Lour root.
文摘鱼藤素是大量存在于豆科植物中的一种鱼藤酮类化合物,具有多种生物学活性,如杀虫、抗肿瘤、抗炎、抗病毒、抗糖尿病神经病变以及抗骨质疏松等。然而,高剂量的鱼藤素可导致呼吸抑制、心脏毒性和神经传导阻断等剂量相关的不良影响,这推动了负载鱼藤素的新制剂和鱼藤素结构修饰类似物的不断发展。本文通过检索SciFinder、Web of science、PubMed、CNKI等数据库中已发表的关于鱼藤素及其衍生物的相关文献资料,对鱼藤素的来源、生物活性、毒性、及其衍生物的研究进展,特别是针对其抗肿瘤活性的结构修饰与优化研究进行了综述,经分析和归纳总结发现针对鱼藤素的结构修饰主要集中于B、C、E环骨架和A环上的取代基,其目的主要是提高抗肿瘤活性并降低毒性,所得衍生物多数是作为Hsp90 C端抑制剂而表现出优良的抗肿瘤活性。本综述研究将为后续基于鱼藤素的生物活性研究和新药研发,特别是关于鱼藤素及其衍生物在抗肿瘤领域的深入研究和探索提供一定的借鉴和参考。
文摘Under the guide of living thing active trace,active ingredients having poisonous effect on frematodes grandis and pieris rapae were extracted from amorpha fruitcosa leaves with CH3CH2OH.Five pure compounds were separated and obtained through purification by column and thin-layer chromatography:6α,12α-Dehgdro-deguelin,6α,12α-Dehgdro-α-toxicarol,（±）-Tephrosin,（-）6-Hgdroxg-6α,12α-Dehydrol-toxicarol and Rotenone.
